Synthesis and Evaluation of 4-Thiazolidinone Derivatives of Naproxen
Design, Synthesis and Acute Anti-Inflammatory Evaluation of New NSAIDs A Having 4-Thiazolidinone Pharmacophore
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NSAIDs represent one of the most widely used drugs, and are used primarily for the treatment of rheumatoid arthritis. the use of NSAIDs is limited by their ability to induce the formation of erosions and ulcers in GIT. The inhibition of COX-2 produced the therapeutic anti-inflammatory action of NSAIDs, while the undesired side effects arise from inhibition of COX-1 activity. Thus, COX-2 selective inhibitors would have reduced side effects. Inhibition of COX-2 is due to the additional space in the COX-2 hydrophobic channel, as well as to the presence of a side pocket in the channel therefore, a...
NSAIDs represent one of the most widely used drugs, and are used primarily for the treatment of rheumatoid arthritis. the use of NSAIDs is limited by their ability to induce the formation of erosions and ulcers in GIT. The inhibition of COX-2 produced the therapeutic anti-inflammatory action of NSAIDs, while the undesired side effects arise from inhibition of COX-1 activity. Thus, COX-2 selective inhibitors would have reduced side effects. Inhibition of COX-2 is due to the additional space in the COX-2 hydrophobic channel, as well as to the presence of a side pocket in the channel therefore, a group of (4-thiazolidinone) pharmacophore incorporated to the naproxen; to increase its size were designed, synthesized and evaluated as potential anti-inflammatory agents with expected inhibitory selectivity toward COX-2 enzyme. Purity and characterization of the synthesized compounds were confirmed by determination of physical properties (melting points & Rf values), (FT-IR), (1H-NMR) spectroscopy and elemental microanalysis. Compounds (Va-e) exhibited higher anti-inflammatory effect than naproxen (50mg/kg, i.p.) at 180-240 min., while compound Vf exhibited lower anti-inflammatory effects.
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